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口服抗假单胞菌化合物CI-919(AT-2266)的体外活性

In vitro activity of CI-919 (AT-2266), an oral antipseudomonal compound.

作者信息

Chartrand S A, Scribner R K, Weber A H, Welch D F, Marks M I

出版信息

Antimicrob Agents Chemother. 1983 May;23(5):658-63. doi: 10.1128/AAC.23.5.658.

Abstract

We tested CI-919 (AT-2266), a nalidixic acid analog, against 555 gram-positive and gram-negative bacteria, using microbroth or agar dilution methods. The activity of CI-919 was compared with those of cephalosporins, tobramycin, ticarcillin, dicloxacillin, rifampin, chloramphenicol, ampicillin, and trimethoprimsulfamethoxazole. The minimal inhibitory concentrations of CI-919 for 90% of isolates were (in micrograms per milliliter): Pseudomonas spp. (including Pseudomonas aeruginosa), 4.0; Enterobacteriaceae, 0.5; Staphylococcus spp., 2.0; Haemophilus influenzae, 0.12; Campylobacter jejuni, 0.12; and enterococci, 16. The minimal inhibitory concentrations of CI-919 for 90% of 82 tobramycin-resistant, gram-negative strains was 4.0 micrograms/ml. CI-919 was bactericidal for most isolates, showing no cross-resistance with unrelated antimicrobial agents, and was stable for 11 weeks at temperatures ranging from 22 to -70 degrees C. Inoculum size and media pH had little effect on the antibacterial activity of CI-919 for nine strains tested. CI-919 may be useful as an oral antibiotic for the treatment of infections due to diverse bacteria, including P. aeruginosa.

摘要

我们使用微量肉汤或琼脂稀释法,对萘啶酸类似物CI-919(AT-2266)针对555株革兰氏阳性和革兰氏阴性细菌进行了测试。将CI-919的活性与头孢菌素、妥布霉素、替卡西林、双氯西林、利福平、氯霉素、氨苄西林和甲氧苄啶磺胺甲恶唑的活性进行了比较。CI-919对90%分离株的最低抑菌浓度(以微克/毫升计)为:假单胞菌属(包括铜绿假单胞菌),4.0;肠杆菌科,0.5;葡萄球菌属,2.0;流感嗜血杆菌,0.12;空肠弯曲菌,0.12;肠球菌,16。CI-919对82株耐妥布霉素革兰氏阴性菌株中90%的最低抑菌浓度为4.0微克/毫升。CI-919对大多数分离株具有杀菌作用,与不相关抗菌药物无交叉耐药性,并且在22至 -70摄氏度的温度范围内可稳定11周。接种量和培养基pH值对测试的9株菌株的CI-919抗菌活性影响很小。CI-919可用作口服抗生素,用于治疗包括铜绿假单胞菌在内的多种细菌引起的感染。

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